Imaging Beta-Amyloid Peptides and Inhibition of Beta-Amyloid Peptide Aggregation

A method for treatment and/or prevention of beta-amyloid (Aβ) peptides aggregation-associated diseases by using carbazole-based fluorophores comprising formula S or V series,

• said method comprising:
• binding said carbazole-based fluorophores to Aβ peptides, oligomers and fibrils thereof;
• inhibiting the growth and/or aggregation of said Aβ peptides, oligomers and/or fibrils upon said binding;
• and
• protecting neuronal cells against the neurotoxic activities of the Aβ oligomers and/or fibrils;
• wherein in said carbazole-based fluorophores, Ar is a heteraromatic ring selected from the group consisting of pyridinyl, substituted pyridinyl, quinolinyl, substituted quinolinyl, acridinyl, substituted acridinyl, benzothiazolyl, substituted benzothiazolyl, benzoxazolyl, and substituted benzoxazolyl;
• R1 is selected from the group consisting of polyethylene glycol chain, alkyl, substituted alkyl, peptide chain, glycosidyl, and C(O)NHCH((CH2CH2O)2CH3)2;
• R2 is selected from the group consisting of ethenyl, ethynyl, azo and azomethinyl.
• R3 is selected from the group consisting of alkyl, HO-alkyl, HS-alkyl, H2N-alkyl, HNalkyl-alkyl, HOOC-alkyl, (alkyl)3N+-alkyl, and (Ph)3P+-alkyl;
• and
• X is selected from the group consisting of F−, Cl−, Br−, I−, HSO4−, H2PO4−, HCO3−, tosylate, and mesylate.